An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

Scott, Fraser J., Puig-Sellart, Mireia, Khalaf, Abedawn I., Henderson, Catherine J., Westrop, Gareth, Watson, David G., Carter, Katharine, Grant, M. Helen and Suckling, Colin J. (2016) An evaluation of Minor Groove Binders as anti-lung cancer therapeutics. Bioorganic & Medicinal Chemistry Letters, 26 (15). pp. 3478-3486. ISSN 0960-894X

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Abstract

A series of 47 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for anti-lung cancer activity by screening against the melanoma cancer cell line B16-F10. Five compounds have been found to possess significant activity, more so than a standard therapy, Gemcitabine. Moreover, one compound has been found to have an activity around 70-fold that of Gemcitabine and has a favourable selectivity index of greater than 125. Furthermore, initial studies have revealed this compound to be metabolically stable and thus it represents a lead for further optimisation towards a novel treatment for lung cancer

Information

URI:

https://eprints.hud.ac.uk/id/eprint/32646

URI:

https://eprints.hud.ac.uk/id/eprint/32646

Title:

An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

Creators:

Scott, Fraser J., Puig-Sellart, Mireia, Khalaf, Abedawn I., Henderson, Catherine J., Westrop, Gareth, Watson, David G., Carter, Katharine, Grant, M. Helen and Suckling, Colin J.

Identification Number:

10.1016/j.bmcl.2016.06.040

Official URL:

https://doi.org/10.1016/j.bmcl.2016.06.040

Date:

1 August 2016

Subjects:

Q Science > QD Chemistry

Schools:

School of Applied Sciences

Library

Item Type: